Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors

Inspired by the thiazole–thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be...

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Published inACS medicinal chemistry letters Vol. 5; no. 6; pp. 628 - 633
Main Authors Chen, Fei, Chai, Hui, Su, Ming-Bo, Zhang, Yang-Ming, Li, Jia, Xie, Xin, Nan, Fa-Jun
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 12.06.2014
Amer Chemical Soc
Subjects
Chemistry, Medicinal
Letter
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
bisthiazole
Histone deacetylase inhibitors
largazole
HDAC INHIBITORS
SAHA
APOPTOSIS
MECHANISM
CONCISE TOTAL-SYNTHESIS
INDUCTION
TRICHOSTATIN-A
LARGAZOLE ANALOGS
BIOLOGICAL EVALUATION
DERIVATIVES
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Summary:Inspired by the thiazole–thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.
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ISSN:1948-5875
1948-5875
DOI:10.1021/ml400470s